1. Neuronal Signaling Apoptosis Immunology/Inflammation NF-κB MAPK/ERK Pathway
  2. Cholinesterase (ChE) Apoptosis Bcl-2 Family Caspase Interleukin Related TNF Receptor Toll-like Receptor (TLR) MyD88 NF-κB p38 MAPK
  3. Chuanbeinone

Chuanbeinone (22-Epidelavinone) 是一种具有口服活性生物碱,被发现存在于 Fritillaria pallidiflora 中。Chuanbeinone 对多种癌细胞具有细胞毒性,可诱导细胞凋亡 (apoptosis) 及 S 期阻滞。Chuanbeinone 可下调 Bcl-2、上调 Bax 并激活 caspase-3。Chuanbeinone 可通过减少促炎细胞因子 (IL-1βIL-6TNF-α) 的产生与 mRNA 表达,同时抑制 TRIFMyD88NF-κBMAPK 依赖的信号通路,发挥抗炎及镇咳作用。Chuanbeinone 可抑制 AChEBChE,其 IC50 值分别为 7.7 和 0.7 μM。Chuanbeinone 可用于肺癌、咳嗽及炎症性疾病的研究。

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Chuanbeinone

Chuanbeinone Chemical Structure

CAS No. : 103530-47-8

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Chuanbeinone (22-Epidelavinone) is an orally active alkaloid found in Fritillaria pallidiflora. Chuanbeinone shows cytotoxicity against mutiple cancer cells and can induces apoptosis and S phase arrest. Chuanbeinone downregulates Bcl-2, upregulates Bax, and activates caspase-3. Chuanbeinone exerts anti-inflammatory and antitussive effects by reducing pro-inflammatory cytokine (IL-1β, IL-6 and TNF-α) production and mRNA expression, and inhibiting TRIF-, MyD88-, NF-κB-, and MAPK-dependent signaling pathways. Chuanbeinone inhibits AChE and BChE with IC50 values of 7.7 and 0.7 μM. Chuanbeinone can be used for the researches of lung carcinoma, cough, inflammatory diseases[1][2][3][4].

IC50 & Target[1]

BChE

0.7 μM (IC50)

AChE

7.7 μM (IC50)

Bax

 

Bcl-2

 

Caspase 3

 

IL-1β

 

IL-6

 

体外研究
(In Vitro)

Chuanbeinone 可抑制 LLC、A2780、HepG2 和 A549 细胞的增殖,其对应的 IC50 值分别为 10.51 μg/mL、18.16 μg/mL、37.97 μg/mL 和 43.74 μg/mL[1]
Chuanbeinone (5-15 μg/mL;48 h) 可在 LLC 细胞中诱导剂量依赖性细胞凋亡,细胞凋亡率为 12.8% 至 64.8%[1]
Chuanbeinone (10 μg/mL;24-72 h) 可在 LLC 细胞中诱导时间依赖性的 S 期阻滞,G0/G1 期的细胞数量减少[1]
Chuanbeinone (5-15 μg/mL;48 h) 可下调 LLC 细胞中的 Bcl-2、上调 Bax 并激活 caspase-3[1]
Chuanbeinone (20-100 μM;24 h) 降低 RAW 264.7 细胞活力[2]
Chuanbeinone (5-20 μM;与 0.2 μg/mL LPS 共处理 24 h) 可通过减少促炎细胞因子的产生与 mRNA 表达,以及抑制 TRIF-、MyD88-、NF-κB-和 MAPK 依赖的信号通路,对 LPS (HY-D1056) 诱导的 RAW 264.7 细胞发挥抗炎作用[2]
Chuanbeinone 对 AChE 的抑制作用 IC50 为 7.7 ± 0.001 μM,对 BChE 的抑制作用 IC50 为 0.7 ± 0.001 μM,且在 100 μM 浓度下表现出 70.7 ± 3.3%的酶抑制率[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: LLC
Concentration: 10 μg/mL
Incubation Time: 24, 48, 72 h
Result: Caused time-dependent accumulation of LLC cells in the S phase, accompanied by a decrease in G0/G1 phase cells.
Increased the sub-G1 population (apoptotic DNA fragmentation) over time.

Western Blot Analysis[1]

Cell Line: LLC
Concentration: 5, 10, 15 μg/mL
Incubation Time: 48 h
Result: Reduced expression of antiapoptotic Bcl-2 and increased expression of proapoptotic Bax (elevating the Bax/Bcl-2 ratio).
Increased levels of cleaved caspase-3 in a dose-dependent manner.

ELISA Assay[2]

Cell Line: RAW 264.7 cells
Concentration: 5, 10, 20 μg/mL
Incubation Time: 24 h co-treated with 0.2 μg/mL LPS
Result: Reduced NO, IL-1β, IL-6 and TNF-α production and mRNA expression.

Western Blot Analysis[2]

Cell Line: RAW 264.7 cells
Concentration: 5, 10, 20 μg/mL
Incubation Time: 24 h co-treated with 0.2 μg/mL LPS
Result: Reduced TRIF, MyD88, NF-κB, and MAPK levels.
体内研究
(In Vivo)

Chuanbeinone (10-40 mg/kg;口服;每日一次;连续 10 天) 在荷 LLC 的 C57BL/6J 小鼠和荷 S180 的 ICR 小鼠中展现出显著的抗肿瘤活性,诱导肿瘤生长抑制、细胞凋亡以及血管生成抑制[1]
Chuanbeinone (1.5-3.0 mg/kg; 口服.; single dose) 在小鼠氨气诱导咳嗽模型中呈现出剂量依赖性的镇咳作用,其中 3.0 mg/kg 剂量可使咳嗽频率被抑制 60.49%[4]
Chuanbeinone (3.0 mg/kg;口服;单次给药) 在小鼠气管酚红分泌模型中未表现出显著的祛痰活性[4]
Chuanbeinone (1.5-3.0 mg/kg; 口服; single dose) 在二甲苯诱导的小鼠耳肿胀模型中,3.0 mg/kg 剂量时可发挥抗炎作用,肿胀抑制率达 37.08%[4]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: LLC-bearing C57BL/6J and S180-bearing ICR mice (male, 18-22 g)[1]
Dosage: 10, 20, 40 mg/kg
Administration: P.o.; daily; 10 days
Result: Achieved 40.97% and 39.15% tumor growth inhibition rate.
Increased TUNEL-positive apoptotic cell number in tumor tissues.
Reduced microvessel density via decreased CD31 expression.
Increased cleaved caspase-3 expression in tumor tissues compared to the control group.
Animal Model: Kunming mice (either sex, 18-22 g)[4]
Dosage: 1.5, 3.0 mg/kg
Administration: P.o.; single dose
Result: Increased cough latent period to 58.20 ± 10.64 s at 3.0 mg/kg.
Reduced cough frequency to 24.30 ± 4.84 (60.49% inhibition) at 3.0 mg/kg.
Reduced cough frequency to 30.16 ± 5.29 (52.68% inhibition) at 1.5 mg/kg.
分子量

413.64

Formula

C27H43NO2

CAS 号
结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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